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Risperidone

Risperidone manual Chemical Properties Uses Benefits and side effects Effect medicine interactions production method Effective dose of Risperidone maintenance therapy reduces relapse rate of schizophrenia
Risperidone
Risperidone structure
CAS No.
106266-06-2
Chemical Name:
Risperidone
Synonyms
Spiron;R-64766;BELIVON;CS-2004;Rispadal;Apexidone;Psychodal;RISPERDAL;RISPERIDAL;Risoeridone
CBNumber:
CB9131730
Molecular Formula:
C23H27FN4O2
Formula Weight:
410.48
MOL File:
106266-06-2.mol

Risperidone Properties

Melting point:
170°C
Boiling point:
572.4±60.0 °C(Predicted)
Density 
1.38±0.1 g/cm3(Predicted)
Flash point:
9℃
storage temp. 
2-8°C
solubility 
DMSO: ≥5mg/mL
pka
pKa 8.3 (Uncertain)
form 
powder
color 
white to off-white
Water Solubility 
44.74mg/L(25 ºC)
Merck 
14,8233
CAS DataBase Reference
106266-06-2(CAS DataBase Reference)
FDA UNII
L6UH7ZF8HC
NCI Dictionary of Cancer Terms
Risperdal; risperidone
ATC code
N05AX08
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS02,GHS06,GHS08
Signal word  Danger
Hazard statements  H225-H301+H311+H331-H370-H301
Precautionary statements  P210-P260-P280-P301+P310-P311
Hazard Codes  T,F
Risk Statements  25-39/23/24/25-23/24/25-11
Safety Statements  28-36-45-36/37-16
RIDADR  3249
WGK Germany  3
RTECS  UV1164800
HazardClass  6.1(a)
PackingGroup  II
HS Code  29333990
Toxicity LD50 in male, female mice, rats, dogs (mg/kg): 29.7, 26.9, 34.3, 35.4, 14.1, 18.3 i.v.; 82.1, 63.1, 113, 56.6, 18.3, 18.3 orally (Janssen, 1988)

Risperidone price More Price(13)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich R-006 Risperidone solution 1.0?mg/mL in methanol, ampule of 1?mL, certified reference material, Cerilliant? 106266-06-2 1 mL $86.6 2021-03-22 Buy
Sigma-Aldrich PHR1631 Risperidone Pharmaceutical Secondary Standard; Certified Reference Material 106266-06-2 500mg $154 2021-03-22 Buy
Sigma-Aldrich 1604654 Risperidone United States Pharmacopeia (USP) Reference Standard 106266-06-2 100mg $366 2021-03-22 Buy
TCI Chemical R0087 Risperidone >98.0%(HPLC)(T) 106266-06-2 50mg $12 2021-03-22 Buy
TCI Chemical R0087 Risperidone >98.0%(HPLC)(T) 106266-06-2 500mg $61 2021-03-22 Buy

Risperidone Chemical Properties,Uses,Production

Risperidone manual

Characters: 1mg Risperidone tablets are white film-coated tablets, after removing the coating ,they are white; 2mg Risperidone tablets are pale orange film-coated tablets,after removing the coating , they are white.
Pharmacological characteristics: This product is benzisoxazole derivative,it is a new generation of antipsychotics. Its active ingredient Risperidone  is a selective monoamine antagonist with unique properties, it has a high affinity with the serotonin 5-HT2 receptors and the dopamine D2 receptors . Risperidone can also be combined with α1-adrenergic receptors  , and it can combine with the histamine H1-receptors and α2-adrenoceptors  with lower affinity . Risperidone can not combine with cholinergic receptors. Risperidone is a potent D2 antagonist, which can improve the positive symptoms of schizophrenia, but inhibition of motor function, as well as  catalepsy caused by it are lesser than classical antipsychotics. Balance of serotonin and dopamine antagonism of the central nervous systemcan can reduce the potential for extrapyramidal side effects, and  expand its role in the treatment of negative symptoms and affective symptoms of schizophrenia.
Pharmacokinetic characteristics: after oral administration,Risperidone can be completely absorbed and the peak of plasma concentration is reached within 1-2 hours, and its absorption is not affected by food. In vivo, Risperidone is metabolized to 9-hydroxy portion-Risperidone, which has similar pharmacological effects to Risperidone. This product can be quickly distributed in the body, Risperidone plasma protein binding rate is 88%, 9-hydroxy-Risperidone plasma protein binding rate is 77%. The drug elimination half-life is about three hours, antipsychotic active ingredient elimination half-life is 24 hours. Most patients reach a steady state of Risperidone in a day, and after 4-5 days ,they reach the 9-hydroxy-risperidone homeostasis. One week after treatment, 70% of the drug  is excreted in urine and 14% of the drug is through fecal excretion, 35-45% of the section of urinary excretion are Risperidone and 9-hydroxy-risperidone, the remaining is non-active metabolite . Elderly patients and patients with renal insufficiency have higher plasma concentrations of Risperidone, so they have slower clearance.

Chemical Properties

It is obtained from dimethylformamide-isopropyl crystallization, m.p. 170.0 ℃. Acute toxicity LD50 male and female mice, male and female rats, male and female dogs (mg/kg): 29.7,26.9,34.3,35.4,14.1,18.3 intravenous injection; 82.1,63.1,113,56.6,18.3,18.3 oral.

Uses

1. It has antagonism effect on 5HT2 receptors and D2 receptors. It is used for acute and chronic schizophrenia.
2. Antipsychotic drugs.

Benefits and side effects

Risperidone advantages:
(1)it is effective not only for positive symptoms, but also  effective for negative symptoms, it can also improve cognitive disorders, thereby improving the patient's condition as a whole.
(2) adverse reactions of the drug is light,it  produces fewer extrapyramidal side effects.
(3)it is easy to adjust the dose, for most patients, the dose is 2~6mg/d, which can produce a therapeutic effect.
(4) for some poor therapeutic effect of conventional antipsychotics or intolerant patients, Risperidone may produce better results.
(5)Compliance of patients  greatly increases during the period of medication .
(6) foreign research shows, Risperidone  can reduce the expenses of patients and reduce the overall expenditure of the patients, and thus more in line with the principles of health economics.
Risperidone side effects:
Risperidone common adverse reactions: insomnia, anxiety, agitation, headache; rare adverse reactions are: drowsiness, fatigue, dizziness, decreased attention, constipation, indigestion, nausea, vomiting, abdominal pain, blurred vision, priapism, erectile dysfunction, weak ejaculation, sexual apathy, urinary incontinence, rhinitis, rash and other allergic reactions. Risperidone can cause extrapyramidal side effects, tremors, rigidity, salivation, bradykinesia, akathisia, acute dystonia, orthostatic hypotensionlactation,lactation, gynecomastia, menstrual disorders, amenorrhea can occur occasionally, Risperidone can also cause weight gain, edema, and increased liver enzymes and so on.

Effect

It is used for the treatment of acute and chronic schizophrenia and other various psychotic state  obvious positive symptoms (such as hallucinations, illusions, thought disorder, hostility, suspicion) and significant negative symptoms (such as unresponsiveness, emotional apathy and social apathy, of few words). Also it can alleviate affective symptoms associated with schizophrenia (such as: depression, guilt, anxiety).  For  patients whom  Risperidone is effective to for acute treatment ,in the maintenance phase of treatment, the Risperidone can continue to play its clinical efficacy.

medicine interactions

1. It can antagonize levodopa and other dopamine agonists role.
2. carbamazepine and other hepatic enzyme inducers may reduce the plasma concentration of the active ingredient of the product, once stop using carbamazepine or other hepatic enzyme inducers, the product should be re-determined its dose ,reduction if necessary .
3. phenothiazines, tricyclic antidepressants, and some β-blockers may increase the plasma concentration of this product, but they do not increase the plasma concentration of the antipsychotic active ingredient.
4. When taken together with other highly protein bound drugs , there is no clinically significant mutual replacement of plasma protein.

production method

1-Acetyl-4-methyl-piperidine chloride and difluorobenzene react under aluminum trichloride catalysis, after acylation, use hydrochloric acid hydrolysis to deacetylate in piperidine ring, and then after hydroxylamine ,use base to catalyze, after cyclization , get benzisoxazole derivatives. 4.4 parts of the isoxazole derivatives, 5.3 parts of ethyl 3-chloro-2-methyl-4H-pyrido [1,2-α] pyrimidin-4-one hydrochloride, 8 parts of sodium carbonate and 0.1 parts of potassium iodide, in dimethyl formamide , heat at 85-90 ℃, Risperidone is generated, 46% yield.

Effective dose of Risperidone maintenance therapy reduces relapse rate of schizophrenia

For treatment of newly diagnosed or recurrent acute schizophrenia, new antipsychotic efficacy are good, but the current maintenance therapy for acute treatment duration and dose has not yet been unified global consensus. This study is designed to investigate, ,the effects that the use of an effective dose of Risperidone maintenance treatment for different time have on disease recurrence after the acute phase treatment of schizophrenia patients is completed , and  verify the safety and tolerability long-term treatment with  Risperidone.
The multicenter open randomized controlled study is participated by the National 19 psychiatric hospitals or psychiatric general hospitals,  Objects of study are  patients in line with the American Diagnostic and Statistical Manual Mental Disorders 4th edition (DSM-Ⅳ) schizophrenia diagnostic criteria , with previous episodes at least once,the total treatment time from this episode to join to the group, is ≤5 months,and they have been completed acute treatment and the symptoms are under control, they have been using fixed-dose Risperidone monotherapy for at least 4 weeks.Exclude patients use Risperidone in combination with  other antipsychotic drugs 30 days prior to enrollment .
Patients are randomly divided into three groups, four weeks reduction groups: the group continue  to receive the effective dose of the acute phase for 4 weeks, followed by 8 weeks when the dose is gradually reduced to 1/2 of the original amount of treatment, followed by four weeks when doctors are allowed according to the patient's condition, efficacy and tolerability to decide whetherthe dose is further reduced to 1/4 of the original amount of treatment and to maintain this dose until the end of the study. 26 weeks reduction group: the group continue  to receive an effective dose of the acute phase of treatment for 26 weeks, followed by the same manner as in group A the dose is reduced and maintained to the end of treatment research. Continuous dose group: Use the effective dose of acute phase of treatment ,there is no reduction throughout the study period.
The results show that using time to recurrence or relapse rate as the evaluation index, continuing with an effective dose of the acute phase of treatment for 4 weeks and 26 weeks , then reducing the dose, can not effectively reduce the recurrence rate. A group has the highest risk of recurrence which is 31.5%, and the results are very similar to those in Cscernansky  reports(  risk of recurrence using Risperidone for 28 months is 34%).  A long time for maintenance treatment or when continuing without reduction can reduce the risk of recurrence . Kane, etc. Using different doses of haloperidol decanoate maintenance therapy for 1 year ,finds that as the dose increases, relapse rate tends to decrease. The use of long-acting drugs actually  ensures that the dose is sustained,which also shows a lower relapse rate which is consistent with the results of this study.
Studies have shown that after acute schizophrenia treatment, continue use of Risperidone in the acute phase of an effective dose without reduction maintenance therapy, which has the lowest risk of relapse and improves the symptoms  further, and does not increase  relatively common weight gain, extrapyramidal symptoms and menstrual disorders and so on significantly. These results indicate that, in order to reduce the relapse rate in patients with acute schizophrenia, the use of an effective dose of Risperidone maintenance treatment ≥6 months is necessary.

Description

Risperidone is a novel antipsychotic introduced for the treatment of acute and chronic schizophrenia. It has a balanced serotonin 5-HT2 and dopamine D2 receptor antagonist activity. While the anti-D2 activity may relate to the antipsychotic potency of neuroleptic agents, an antidepressive efficacy of substances with anti-5-HT2 activity has been suggested. Risperidone, therefore, has therapeutic action on both positive and negative symptoms of schizophrenia and produces significantly fewer side effects especially extrapyramidal symptoms compared with commonly used pure D2 antagonist antipsychotics. It also has potential for management of alcohol withdrawal and cocaine addiction.

Chemical Properties

Crystalline Solid

Originator

Janssen (U.S.A.)

Uses

neuroprotectant, inhibitory neurotransmitter, GABA agonist

Uses

For the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropria

Uses

A combined serotonin (5-HT2) and dopamine (D2) receptor antagonist

Definition

ChEBI: A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.

brand name

Risperdal (Janssen).

General Description

Risperidone (Risperdal, a benzisoxazole)has the structural features of a hybrid molecule between abutyrophenone antipsychotic and a trazodone-like antidepressant.Its superior side effects profile (compared withhaloperidol) at dosage of 6 mg/d or less and the lower riskof tardive dyskinesia have contributed to its very widespreaduse. It benefited refractory psychotic patients, withparkinsonism controlled at one tenth the dose of antiparkinsoniandrugs used with haloperidol.Coexisting anxietyand depressive syndromes were also lessened. It is reportedto decrease the negative (e.g., withdrawal, apathy) as well asthe positive (e.g., delusions, hallucinations) symptoms ofschizophrenia. This is reportedly a consequence of the compound’scombination 5-HT2–D2 receptor antagonistic properties.Overall, the reasons for the decreased EPS and effectiveness against negative symptom are still under investigation.It is an important atypical antipsychotic.Risperidone is metabolized in the liver by CYP2D6 to anactive metabolite, 9-hydroxyrisperidone. Because thismetabolite and risperidone are nearly equipotent, the clinicalefficacy of the drug reflects both compounds.

General Description

Risperidone, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2]pyrimidin-4-one (Risperdal), is awhite to slightly beige powder that is essentially insoluble inwater. Risperidone is also available as a 1-mg/mL oral solutionand as orally disintegrating tablets (Risperdal M-Tab).Risperidone is well absorbed, and peak levels occur about 1hour after administration. The absorption of risperidone is notaffected by food. Risperidone is about 90% bound to albuminand 1-acid glycoprotein, whereas its metabolite 9-hydroxyrisperidoneis bound about 77%. Risperidone is primarilymetabolized in humans to the active metabolite 9-hydroxyrisperidone..The major side effects associated with risperidonetherapy are orthostatic hypotension, dose-related hyperprolactinemia,mild weight gain, EPS, and insomnia.Athigher doses (6 mg/day), risperidone is the atypical antipsychoticthat most closely resembles conventional agents. APET study in a group of individuals with schizophreniashowed that D2 receptor occupancy was dose dependent. Ifthe dose was increased such that D2 receptor occupancy was79% to 85%, the majority of patients developed EPS.Risperidone is associated with increased mortality in elderlypatients with dementia-related psychosis and is not recommendedfor these individuals.23 Risperidone binds with highaffinity at 5-HT2A, 5-HT7, D2, 1, 2, and H1 receptors. Theantipsychotic action of risperidone has been proposed tobe the result of D2 and 5-HT2A antagonism.

Biological Activity

Atypical antipsychotic agent that displays 5-HT 2A receptor antagonism. Also displays high affinity at D 2 receptors (K i values are 0.4 and 3.13 nM for 5-HT 2A and D 2 receptors respectively).

Risperidone Preparation Products And Raw materials

Raw materials

Preparation Products


Risperidone Suppliers

Global( 446)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-66670886
info@dakenchem.com China 20914 58
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0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
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Guangzhou PI PI Biotech Inc
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020-81716319 sales@pipitech.com;87478684@qq.com China 3245 55
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BOC Sciences
1-631-485-4226
1-631-614-7828 inquiry@bocsci.com United States 19752 58

View Lastest Price from Risperidone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-11-30 Risperidone
106266-06-2
US $806.00 / KG 1KG 99% 100KG Baoji Guokang Bio-Technology Co., Ltd.
2021-11-19 risperidone
US $10.00 / KG 1KG 99.99% 500kg/month Handan Tongyi New Material Technology Co., Ltd
2021-11-19 Risperidone Product
106266-06-2
US $1.00 / KG 1KG 99% 100 Kilogram/Week Handan Tongyi New Material Technology Co., Ltd

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